GPCR Target |
Reference |
Orphans |
Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS, Davenport AP, Brown AJ, Green A, Wigglesworth MJ and Rees S. (2013). Screening β-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. J Biomol Screen 18(5):599-609. |
GPR3 |
Ye C, Zhang Z, Wang Z, Hua Q, Zhang R, Xie X.. (2014).Identification of a novel small-molecule agonist for human G protein-coupled receptor 3. J Pharmacol Exp Ther. 349(3):437-43. |
GPR18 |
Console-Bram L, Brailoiu E, Brailoiu GC, Sharir H, Abood ME. (2014). Activation of GPR18 by cannabinoid compounds: a tale of biased agonism. Br J Pharmacol. 171(16):3908-17. |
GPR18, GPR55 |
Rempel V, Atzler K, Behrenswerth A, Karcz T, Schoeder C, Hinz S, Kaleta M, Thimm D, Kiec-Kononowiczb K, Muller CE (2014). Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55. MedChemComm 5, 632-49. |
GPR18, GPR55 |
Fuchs A, Rempel V and Muller CE. (2013). The natural product magnolol as a lead structure for the development of potent cannabinoid receptor agonists. PLoS One 8(10): e77739. |
GPR32 |
Krishnamoorthy S, Recchiuti A, Chiang N, Fredman G and Serhan CN. (2012). Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs. Am J Pathol 180(5):2018-27. |
GPR32 |
Krishnamoorthy S, Recchiuti A, Chiang N, Yacoubian S, Lee CH, Yang R, Petasis NA and Serhan CN. (2010). Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci USA 107(4):1660-5. |
GPR35 |
MacKenzie AE, Caltabiano G, Kent TC, Jenkins L, McCallum JE, Hudson BD, Nicklin SA, Fawcett L, Lane R, Charlton SJ and Milligan G. (2014). The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35. Mol Pharmacol 85(1):91-104. |
GPR35 |
Neetoo-Isseljee Z, MacKenzie AE, Southern C, Jerman J, McIver EC, Harries N, Taylor DL and Milligan G. (2013). High-throughput identification and characterization of novel, species-selective GPR35 agonists. J Pharmacol 344(3): 568-78. |
GPR35 |
Jenkins L, Alvarez-Curto E, Campbell K, de Munnik S, Canals M, Schlyer S and Milligan G. (2011). Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Galpha(1)(3) and beta-arrestin-2. Br J Pharmacol 162(3):733-48. |
GPR35, GPR55 |
Reggio P, Shore D. (2015). The Therapeutic Potential of Orphan GPCRs, GPR35 and GPR55. Front Pharmacol (review article) 6:69. |
GPR35, GPR55 |
Funke M, Thimm D, Schiedel AC and Muller CE. (2013). 8-benzamidochromen-4-one-2-carboxylic acids - potent and selective agonists for the orphan G protein-coupled receptor GPR35. J Med Chem 56(12):5182-97. |
GPR55 |
Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M and Heinemann A. (2013). A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther 346(1):54-66. |
GPR55 |
Rempel V, Volz N, Gluser F, Nieger M, Bruse S and Muller CE. (2013). Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold. J Med Chem56(11):4798-810. |
GPR55 |
Yamashita A, Oka S, Tanikawa T, Hayashi Y, Nemoto-Sasaki Y, Sugiura T. (2013). The actions and metabolism of lysophosphatidylinositol, an endogenous agonist for GPR55. Prostaglandins Other Lipid Mediat 107:103-16. |
GPR101 |
Cho-Clark M, Larco DO, Semsarzadeh NN, Vasta F, Mani SK, Wu TJ. (2014). GnRH-(1-5) Transactivates EGFR in Ishikawa Human Endometrial Cells via an Orphan G Protein-Coupled Receptor. Mol Endocrinol 28(1):80-98. |
Orphan Panel, GPR173 |
Larco DO, Cho-Clark M, Mani SK and Wu TJ. (2013). The metabolite GnRH-(1-5) inhibits the migration of immortalized GnRH neurons. Endocrinology 154(2):783-95. |
EBI2 (GPR183) |
Gessier F, Preuss I, Yin H, Rosenkilde MM, Laurent S, Endres R, Chen YA, Marsilje TH, Seuwen K, Nguyen DG, Sailer AW (2014). Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor. J Med Chem. 57(8):3358-68. |
EBI2 (GPR183) |
Benned-Jensen T, Norn C, Laurent S, Madsen CM, Larsen HM, Arfelt KN, Wolf RM, Frimurer T, Sailer AW, Rosenkilde MM. (2013). Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183). J Biol Chem 287(42):35470-83. |
EBI2 (GPR183) |
Benned-Jensen T, Madsen CM, Arfelt KN, Smethurts C, Blanchard A, Jepras R, Rosenkilde MM. (2013). Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation. FEBS Open Bio. 19;3:156-60. |
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